Article
The two major imatinib resistance mutations E255K and T315I enhance the activity of BCR/ABL fusion kinase.
Biochemical and biophysical research communications - 9 Jul 2004
Yamamoto Masahide, Kurosu Tetsuya, Kakihana Kazuhiko, Mizuchi Daisuke, Miura Osamu
Abstract excerpt
The resistance to the tyrosine kinase inhibitor imatinib in BCR/ABL-positive leukemias is mostly associated with mutations in the kinase domain of BCR/ABL, which include the most prevalent mutations E255K and T315I. Intriguingly, these mutations have also been identified in some patients before imatinib treatment. Here we examined the effects of these mutations on the kinase activity of a BCR/ABL kinase domain...
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